linagliptin / Generic mfg. 
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  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Clinical, Review, Journal:  Do sulphonylureas still have a place in clinical practice? (Pubmed Central) -  Jul 13, 2019   
    80% of people with diabetes live in low-to-middle income countries, so the effectiveness, affordability, and safety of sulphonylureas are particularly important considerations when prescribing glucose-lowering therapy. Results of ongoing head-to-head studies with new drugs, such as the comparison of glimepiride with linagliptin in the CAROLINA study and the comparison of various therapies (including sulphonylureas) for glycaemic control in the GRADE study, will determine the place of sulphonylureas in glucose-lowering therapy algorithms for patients with type 2 diabetes.
  • ||||||||||  Clinical, Review, Journal:  DPP-4 Inhibition and the Path to Clinical Proof. (Pubmed Central) -  Jul 6, 2019   
    ...This action was seen when DPP-4 inhibitors were used both as monotherapy and as add-on to other therapies, i.e., metformin, sulfonylureas, tiazolidinediones or exogenous insulin...Five of the DPP-4 inhibitors (sitagliptin, vildagliptin, alogliptin, saxagliptin and linagliptin) were approved by regulatory authorities and entered the market between 2006 and 2013...This article summarizes the development of the DPP-4 inhibition concept from its early stages in the 1990s. The article underscores that the development has its basis in scientific studies on pathophysiology of type 2 diabetes and the importance of targeting the islet dysfunction, that the development has been made possible through academic science in collaboration with the research-oriented pharmaceutical industry, and that the development of a novel concept takes time and requires focused efforts, persistence and long-term perserverance.
  • ||||||||||  Review, Journal:  Cardiovascular outcome trials of glucose-lowering medications: an update. (Pubmed Central) -  Jun 26, 2019   
    Three further cardiovascular (CV) outcome studies of glucose-lowering drugs (linagliptin, albiglutide and dapagliflozin) have recently been published, adding to the twelve earlier within-class studies...However, taken together with the findings from two previous studies of DPP4 inhibitors (sitagliptin and saxagliptin), the three DPP4 inhibitor CV outcome trials (CVOTs) have highlighted a safety signal regarding risk of pancreatitis...Despite being a short duration study, albiglutide showed strong superiority for reduction in the major adverse CV events (MACE) composite in people with extant cardiovascular disease (CVD), in line with the earlier studies on the GLP-1 receptor agonists (GLP-1RAs) liraglutide and semaglutide...There is also strong protection against renal decline with dapagliflozin, with similar risk estimates in DECLARE as previously reported for empagliflozin and canagliflozin...In summary, taking into account the findings from these new studies, it is suggested that a GLP-1RA should be offered to all people with CVD and type 2 diabetes, and SGLT2 inhibitors should be prescribed for those at high risk of heart failure or with progressive decline in eGFR. DPP4 inhibitors are a safe choice within the glucose-lowering stepped algorithm.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Clinical, P4 data, Journal:  Post-marketing Study of Linagliptin: A Pilot Study. (Pubmed Central) -  Jun 11, 2019   
    AE occurred in 12 (36.4%) patients, and 16.7% were in monotherapy. Linagliptin did not presented, in real world, the desired performance as showed in randomized premarketing clinical trials and it should be carefully evaluated in public health services.
  • ||||||||||  linagliptin / Generic mfg.
    Trial completion, Trial completion date, Trial primary completion date:  Active Surveillance Research Program for the Assessment of the Safety and the Effectiveness of Linagliptin (clinicaltrials.gov) -  Jun 7, 2019   
    P=N/A,  N=99999, Completed, 
    Linagliptin did not presented, in real world, the desired performance as showed in randomized premarketing clinical trials and it should be carefully evaluated in public health services. Active, not recruiting --> Completed | Trial completion date: May 2019 --> Nov 2018 | Trial primary completion date: May 2019 --> Nov 2018
  • ||||||||||  Xarelto (rivaroxaban) / Bayer, J&J, Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly, Pradaxa (dabigatran etexilate) / Boehringer Ingelheim
    #pradaxa #xarelto #Boehringer #trajenta (Twitter) -  Jun 2, 2019   
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    New trial:  Linagliptin in Post-renal Transplantation (clinicaltrials.gov) -  May 30, 2019   
    P,  N=28, Completed, 
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Clinical, Journal:  Effect of linagliptin on oxidative stress markers in patients with type 2 diabetes: a pilot study. (Pubmed Central) -  May 30, 2019   
    In this study, we demonstrated that linagliptin partially attenuated oxidative stress. We also demonstrated that linagliptin treatment reduced urinary L-FABP excretion, suggesting that renal tubule-interstitial injury may be attenuated by linagliptin (UMIN 000015308).
  • ||||||||||  Journal:  Identification of a Novel Metabolite of Vildagliptin in Humans: Cysteine Targets the Nitrile Moiety to Form a Thiazoline Ring. (Pubmed Central) -  May 29, 2019   
    ...We found that VG and anagliptin (ANG), which both contain a cyanopyrrolidine moiety, rapidly reacted in non-enzymatic manners on co-incubation with l-cysteine...M20.7, sitagliptin, linagliptin, and alogliptin, having no cyanopyrrolidine moiety, were stable on incubation with l-cysteine or GSH...Such binding may lead to unpredictable immune responses in humans. l-Cysteine, rather than GSH, would likely be useful to detect the potential for covalent binding that could initiate immune-mediated hepatotoxicity.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Preclinical, Journal:  Vascular protection of DPP-4 inhibitors in retinal endothelial cells in in vitro culture. (Pubmed Central) -  May 15, 2019   
    Mechanistically, linagliptin potently suppresses TNF-α-induced accumulation of NF-κB nuclear protein p65 and activation of NF-κB promoter. Our data indicate that linagliptin is an anti-inflammatory diabetic agent, with the potential to be applied as a treatment for diabetic retinopathy.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly, Synjardy (empagliflozin/metformin) / Boehringer Ingelheim, Eli Lilly, Jardiance (empagliflozin) / Eli Lilly, Boehringer Ingelheim
    Trial completion date, Trial primary completion date, Real-world evidence, Real-world:  DIA_CENTRAL:T2D Treatment Pattern in Central Europe (clinicaltrials.gov) -  May 14, 2019   
    P=N/A,  N=4000, Not yet recruiting, 
    Our data indicate that linagliptin is an anti-inflammatory diabetic agent, with the potential to be applied as a treatment for diabetic retinopathy. Trial completion date: Aug 2019 --> May 2020 | Trial primary completion date: Aug 2019 --> May 2020
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Clinical, Journal:  Cardiovascular safety of DPP-4 inhibitors compared to that of sulfonylureas (Pubmed Central) -  Apr 28, 2019   
    However, some heterogeneity exists, most probably explained by differences between the molecules, especially among sulfonylureas as those of last generation (more particularly gliclazide) seem to have a better safety profile. The ongoing head-to-head prospective trial CAROLINA compares the cardiovascular safety of glimepiride and linagliptin in high-risk patients, with results expected in 2019.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Clinical, Review, Journal:  Linagliptin safety profile: A systematic review. (Pubmed Central) -  Apr 26, 2019   
    Of the AEs, 14.9 (±3.1)% were associated with the use of linagliptin in monotherapy, and 17.6 (±6.0)% in combination. The linagliptin AEs have a varied occurrence and frequency, ranging from mild to moderate intensity.
  • ||||||||||  Retrospective data, Review, Journal:  Heart Failure Hospitalization with DPP-4 Inhibitors: A Systematic Review and Meta-analysis of Randomized Controlled Trials. (Pubmed Central) -  Apr 25, 2019   
    To note, neither Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS), nor Cardiovascular and Renal Microvascular Outcome Study with Linagliptin (CARMELINA), showed any signals of hHF with these two agents...Meta-analysis of all randomized controlled trials that explicitly looked for hHF for ≥52 weeks (N = 48,199) also did not show any significant increase in hHF (fixed model peto odds ratio 1.05; 95% CI 0.95-1.15, P = 0.36; I: 43.74%, tau: 0.016, P = 0.10). This meta-analysis suggests no significant increase in hHF with DPP-4 inhibitors, although a nonsignificant heterogeneity across the trials might limit this observation.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly, Januvia (sitagliptin) / Merck (MSD)
    Review, Journal:  Using DDP-4 inhibitors to modulate beta cell function in type 1 diabetes and in the treatment of Diabetic Kidney Disease. (Pubmed Central) -  Apr 5, 2019   
    Linagliptin reduces albuminuria and protects renal endothelium from the deleterious effects of hyperglycemia. The effects of DPP-4 inhibitors on preserving beta-cell function in certain sub- types of T1DM [e.g. Latent Autoimmune Diabetes in Adult (LADA) and Slowly Progressive Type 1 Diabetes (SPIDDM)] are encouraging and show promise.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Preclinical, Journal:  Linagliptin protects rat carotid artery from balloon injury and activates the NRF2 antioxidant pathway. (Pubmed Central) -  Mar 29, 2019   
    Moreover, heme oxygenase-1 (HO-1) and NAD(P)H quinine oxidoreductase 1 (NQO1), two downstream targets of NRF2, were further up-regulated after linagliptin treatment compared with injury group. In conclusion, our data suggest that linagliptin protects carotid artery from balloon injury-induced neointima formation and activates the NRF2 antioxidant pathway.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Journal:  Linagliptin Suppresses Electrical and Structural Remodeling in the Isoproterenol Induced Myocardial Injury Model. (Pubmed Central) -  Mar 29, 2019   
    The injured area was reduced in the ISP + Lin group in comparison with the ISP group (P < 0.05). Serum d-ROMs level in acute phase was higher in ISP group than the other 2 groups (sham: 214 ± 55 versus ISP: 404 ± 45 versus ISP + Lin: 337 ± 20 U.CARR, P < 0.05).Linagliptin suppressed structural and electrical changes, possibly through the antioxidative effect, in this myocardial injury model.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly, Januvia (sitagliptin) / Merck (MSD)
    Clinical, Journal:  Effect of Linagliptin and Voglibose on metabolic profile in patients with Type 2 Diabetes: a randomized, double-blind, placebo-controlled trial. (Pubmed Central) -  Mar 27, 2019   
    P4
    Serum d-ROMs level in acute phase was higher in ISP group than the other 2 groups (sham: 214 ± 55 versus ISP: 404 ± 45 versus ISP + Lin: 337 ± 20 U.CARR, P < 0.05).Linagliptin suppressed structural and electrical changes, possibly through the antioxidative effect, in this myocardial injury model. Linagliptin modestly improves glycemic profile in patients with well controlled T2DM; however, it may not have an effect on insulin sensitivity in these patients.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Trial completion date, Trial primary completion date:  PRELLIM: Effect of Linagliptin + Metformin vs Metformin Alone in Patients With Prediabetes (clinicaltrials.gov) -  Feb 27, 2019   
    P4,  N=140, Active, not recruiting, 
    N=292 --> 410 Trial completion date: Aug 2018 --> May 2019 | Trial primary completion date: Oct 2017 --> Mar 2019
  • ||||||||||  Tenelia (teneligliptin) / Daiichi Sankyo, Mitsubishi Tanabe
    Trial completion, Trial completion date, Trial primary completion date, Head-to-Head:  TELIUS: Teneligliptin Versus Linagliptin in Diabetes Mellitus Type Two Patients (clinicaltrials.gov) -  Feb 22, 2019   
    P4,  N=168, Completed, 
    Trial completion date: Aug 2018 --> May 2019 | Trial primary completion date: Oct 2017 --> Mar 2019 Recruiting --> Completed | Trial completion date: Apr 2019 --> Sep 2018 | Trial primary completion date: Jan 2019 --> Sep 2018